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Enhanced Transdermal Permeation Of Bupropion Hydrochloride By Chemical Modification

Author(s): D.P Gondaliya, K Pundarikakshudu

Bupropion, a monocyclic aminoketone is used primarily for the treatment of major depression. On oral administration, the drug undergoes extensive first pass metabolism. Delivery of bupropion via transdermal route would minimize some of the deficiencies associated with the oral delivery. In the present study, effect of various vehicles and penetration enhancers on diffusion kinetics of the salt and free drug through the human cadaver skin was studied using a modified diffusion cell. The diffused drug was quantified by UV spectrophotometry at 298 nm in phosphate buffer saline. A 100-fold increase In permeability rate was observed with free base compared to salt form. As a vehicle, alcohol was found to be superior compared to phosphate buffer saline and propylene glycol in permeation of free base. Permeation was enhanced by up to 30 %with linseed oil and myristic acid when propylene glycol was used as a vehicle. The study provides suitable clues for delivery of bupropion by the transdermal route.


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